{"title":"大鼠大脑皮层[3H]地西帕明结合的药理学特征","authors":"Pavel D. Hrdina","doi":"10.1016/0364-7722(81)90045-X","DOIUrl":null,"url":null,"abstract":"<div><p></p><ul><li><span>1.</span><span><p>1. The specific binding of [<sup>3</sup>H]desipramine to membranes from rat brain cortex is biphasic and the Scatchard analysis of data shows two distinct components: the high affinity component, with a dissociation constant (K<sub>D</sub>) of 4.5 nM and the low affinity component (K<sub>D</sub> = 80 nM).</p></span></li><li><span>2.</span><span><p>2. Different order of potency in displacing the high affinity [<sup>3</sup>H]desipramine and [<sup>3</sup>H]imipramine binding was shown by various compounds tested. Nortriptyline and nisoxetine were the most potent displacers of [<sup>3</sup>H]desipramine specific binding while chlorimipramine and fluoxetine showed highest potency in competing for [<sup>3</sup>H]imipramine binding sites.</p></span></li><li><span>3.</span><span><p>3. Significant correlation was found between the ability of various drugs to inhibit [<sup>3</sup>H]desipramine binding and their potency to block the neuronal uptake of noradrenaline in brain.</p></span></li><li><span>4.</span><span><p>4. The results suggest that the high affinity binding of [<sup>3</sup>H]desipramine is distinct from that of [<sup>3</sup>H]imipramine and is most likely associated with sites involved in neuronal uptake of noradrenaline.</p></span></li></ul></div>","PeriodicalId":20801,"journal":{"name":"Progress in neuro-psychopharmacology","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"1981-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0364-7722(81)90045-X","citationCount":"9","resultStr":"{\"title\":\"Pharmacological characterization of [3H] desipramine binding in rat cerebral cortex\",\"authors\":\"Pavel D. Hrdina\",\"doi\":\"10.1016/0364-7722(81)90045-X\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p></p><ul><li><span>1.</span><span><p>1. The specific binding of [<sup>3</sup>H]desipramine to membranes from rat brain cortex is biphasic and the Scatchard analysis of data shows two distinct components: the high affinity component, with a dissociation constant (K<sub>D</sub>) of 4.5 nM and the low affinity component (K<sub>D</sub> = 80 nM).</p></span></li><li><span>2.</span><span><p>2. Different order of potency in displacing the high affinity [<sup>3</sup>H]desipramine and [<sup>3</sup>H]imipramine binding was shown by various compounds tested. Nortriptyline and nisoxetine were the most potent displacers of [<sup>3</sup>H]desipramine specific binding while chlorimipramine and fluoxetine showed highest potency in competing for [<sup>3</sup>H]imipramine binding sites.</p></span></li><li><span>3.</span><span><p>3. Significant correlation was found between the ability of various drugs to inhibit [<sup>3</sup>H]desipramine binding and their potency to block the neuronal uptake of noradrenaline in brain.</p></span></li><li><span>4.</span><span><p>4. The results suggest that the high affinity binding of [<sup>3</sup>H]desipramine is distinct from that of [<sup>3</sup>H]imipramine and is most likely associated with sites involved in neuronal uptake of noradrenaline.</p></span></li></ul></div>\",\"PeriodicalId\":20801,\"journal\":{\"name\":\"Progress in neuro-psychopharmacology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1981-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0364-7722(81)90045-X\",\"citationCount\":\"9\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Progress in neuro-psychopharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/036477228190045X\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Progress in neuro-psychopharmacology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/036477228190045X","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Pharmacological characterization of [3H] desipramine binding in rat cerebral cortex
1.
1. The specific binding of [3H]desipramine to membranes from rat brain cortex is biphasic and the Scatchard analysis of data shows two distinct components: the high affinity component, with a dissociation constant (KD) of 4.5 nM and the low affinity component (KD = 80 nM).
2.
2. Different order of potency in displacing the high affinity [3H]desipramine and [3H]imipramine binding was shown by various compounds tested. Nortriptyline and nisoxetine were the most potent displacers of [3H]desipramine specific binding while chlorimipramine and fluoxetine showed highest potency in competing for [3H]imipramine binding sites.
3.
3. Significant correlation was found between the ability of various drugs to inhibit [3H]desipramine binding and their potency to block the neuronal uptake of noradrenaline in brain.
4.
4. The results suggest that the high affinity binding of [3H]desipramine is distinct from that of [3H]imipramine and is most likely associated with sites involved in neuronal uptake of noradrenaline.
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